Potent Cyclic Peptide Inhibitors of FXIIa Discovered by mRNA Display with Genetic Code Reprogramming

Daniel J Ford, Nisharnthi M Duggan, Sarah E Fry, Jorge Ripoll-Rozada, Stijn M Agten, Wenyu Liu, Leo Corcilius, Tilman M Hackeng, Rene van Oerle, Henri M H Spronk, Anneliese S Ashhurst, Vishnu Mini Sasi, Joe A Kaczmarski, Colin J Jackson, Pedro José Barbosa Pereira, Toby Passioura, Hiroaki Suga, Richard J Payne

Research output: Contribution to journalArticleAcademicpeer-review

Original languageEnglish
Pages (from-to)7853-7876
Number of pages24
JournalJournal of Medicinal Chemistry
Volume64
Issue number11
DOIs
Publication statusPublished - 10 Jun 2021

Keywords

  • Binding Sites
  • Factor XIIa/antagonists & inhibitors
  • Gene Library
  • Genetic Code
  • Humans
  • Inhibitory Concentration 50
  • Kallikreins/chemistry
  • Molecular Dynamics Simulation
  • Partial Thromboplastin Time
  • Peptides, Cyclic/chemistry
  • Protein Stability
  • Prothrombin Time
  • Puromycin/chemistry
  • RNA, Messenger/chemistry
  • Serine Proteinase Inhibitors/chemistry
  • Structure-Activity Relationship
  • THROMBUS FORMATION
  • MACROCYCLE INHIBITOR
  • IN-VITRO SELECTION
  • VALIDATION
  • COAGULATION-FACTOR XII
  • GENERATION

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